2,5-diketopiperazines as potent and selective oxytocin antagonists - 1: identification, stereochemistry and initial SAR

被引：59
|
作者：
Wyatt, PG
Allen, MJ
Borthwick, AD
Davies, DE
Exall, AM
Hatley, RJD
Irving, WR
Livermore, DG
Miller, ND
Nerozzi, F
Sollis, SL
Szardenings, AK
机构：
[1] GlaxoSmithKline Res & Dev Ltd, Dept Med Chem, CVU UK, Med Res Ctr, Stevenage SG1 2NY, Herts, England
[2] GlaxoSmithKline Res & Dev Ltd, ADCP Harlow Res 2, Harlow CM19 5AW, Essex, England
[3] Affymax Res Inst, Santa Clara, CA 95051 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 10期
关键词：
oxytocin; oxytocin receptor; preterm birth; antagonists; unencoded libraries; 2,5-diketopiperidines; Ugi reaction; screening; pooled libraries; solid phase; structure-activity relationships;
D O I：
10.1016/j.bmcl.2005.03.045
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
This paper covers efforts to discover orally active potent and selective oxytocin antagonists. Screening pooled libraries identified a novel series of 2,5-diketopiperazine derivatives with antagonist activity at the human oxytocin receptor. We report the initial structure-activity relationship investigations and the determination of the stereochemistry of the most potent compounds. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2579 / 2582
页数：4
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